2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]-
- Product Name
- 2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]-
- CAS No.
- 865305-30-2
- Chemical Name
- 2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]-
- Synonyms
- Ro 4;AF 353;CS-2469;CHEMBL526307;AF-353 (Ro-4);AF-353, 10 mM in DMSO;CHEMBL526307;AF 353;AF353;5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidine-2,4-diamine;Ro4,inhibit,AF-353,P2X Receptor,Inhibitor,Ro 4,P2XRs,AF353,AF 353;5-[5-Iodo-4-methoxy-2-(1-methylethyl)phenoxy]-2,4-pyrimidinediamine
- CBNumber
- CB72609596
- Molecular Formula
- C14H17IN4O2
- Formula Weight
- 400.21
- MOL File
- 865305-30-2.mol
2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]- Property
- Boiling point:
- 510.2±60.0 °C(Predicted)
- Density
- 1.619±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 32 mg/mL (79.96 mM)
- pka
- 6.89±0.10(Predicted)
- form
- Solid
- color
- Light brown to brown
- InChI
- InChI=1S/C14H17IN4O2/c1-7(2)8-4-11(20-3)9(15)5-10(8)21-12-6-18-14(17)19-13(12)16/h4-7H,1-3H3,(H4,16,17,18,19)
- InChIKey
- AATPYXMXFBBKFO-UHFFFAOYSA-N
- SMILES
- C1(N)=NC=C(OC2=CC(I)=C(OC)C=C2C(C)C)C(N)=N1
N-Bromosuccinimide Price
- Product number
- 23034
- Product name
- AF-353
- Packaging
- 1mg
- Price
- $32
- Updated
- 2022/04/27
- Product number
- 23034
- Product name
- AF-353
- Packaging
- 5mg
- Price
- $102
- Updated
- 2022/04/27
- Product number
- 23034
- Product name
- AF-353
- Packaging
- 10mg
- Price
- $189
- Updated
- 2022/04/27
- Product number
- 1897CW
- Product name
- 2,4-Pyrimidinediamine,5-[5-iodo-4-methoxy-2-(1-methylethyl)phenoxy]-
- Packaging
- 10mg
- Price
- $245
- Updated
- 2021/12/16
- Product number
- CS-5061
- Product name
- AF-353
- Purity
- 98.95%
- Packaging
- 25mg
- Price
- $310
- Updated
- 2021/12/16
2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]- Chemical Properties,Usage,Production
Description
AF-353 is a noncompetitive dual antagonist of the purinoreceptors P2X3 and P2X2/3 (IC50s = 10 and 79.4 nM, respectively). It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 (IC50 = >10 μM for all). It inhibits calcium flux in CHO-K1 cells expressing the rat P2X3 receptor and in 1321N1 cells expressing the human P2X3 and P2X2/3 receptors (IC50s = 8.91, 8.71, and 38.9 nM, respectively). AF-353 decreases the electrical signals in the detrusor, but not striated, muscle of the bladder in female rats.
Uses
AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3[1][2].
in vivo
AF-353 (Ro-4) does not compromise oxygen levels or cardiac function[2].
AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) inhibits the purinergic response in both normal and spinal cord-injured (SCI) rats[2].
AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) also reduces the inter-contractile interval in normal but not in SCI rats; however, the frequency of non-voiding (NVC) in SCI rats is significantly reduced[2].
| Animal Model: | Female Sprague-Dawley rats (250–300 g) bearing SCI[2] |
| Dosage: | 10 mg/kg, 20 mg/kg |
| Administration: | Intravenous injection; interval of 90 minutes, for 4 hours to 6 hours |
| Result: | Significantly reduced purinergic response in both normal and SCI rats. |
IC 50
P2X3 Receptor
References
[1] Gever JR, et al. AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist. Br J Pharmacol. 2010 Jul;160(6):1387-1398. DOI:10.1111/j.1476-5381.2010.00796.x
[2] Munoz A, et al. Modulation of bladder afferent signals in normal and spinal cord-injured rats by purinergic P2X3 and P2X2/3receptors. BJU Int. 2012 Oct;110(8 Pt B):E409-414. DOI:10.1111/j.1464-410X.2012.11189.x
2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]- Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from 2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]- manufacturers
- Product
- af-353 865305-30-2
- Price
- US $100.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 100KG
- Release date
- 2021-09-13
- Product
- af-353 865305-30-2
- Price
- US $100.00/Kg/Bag
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 10kg
- Release date
- 2021-09-15